273217-89-3Relevant academic research and scientific papers
SUBSTITUTED UREA DERIVATIVES AND PHARMACEUTICAL USES THEREOF
-
Paragraph 0312; 3013; 0531; 0532, (2017/12/15)
The present invention is involved in substituted urea derivatives and pharmaceutical uses thereof. Specifically, the present invention provides the mentioned substituted urea derivatives, and its stereoisomer, geometric isomer, tautomer, nitroxide, hydrate, solvate, metabolism product, ester, and pharmaceutically acceptable salt or its prodrug. The present invention also provides the medicament composition comprising the mentioned substituted urea derivatives, and uses of the mentioned substituted urea derivatives or medicament composition in the protection, treatment, curing, or relief of the proliferative diseases of patients, and its use in regulating the activity of protein kinase.
TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
-
Paragraph 0804; 0805, (2016/12/22)
Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
Labeeuw, Olivier,Levoin, Nicolas,Poupardin-Olivier, Olivia,Calmels, Thierry,Ligneau, Xavier,Berrebi-Bertrand, Isabelle,Robert, Philippe,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
, p. 2548 - 2554 (2013/06/27)
Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis
Procopiou, Panayiotis A.,Browning, Christopher,Buckley, Jennifer M.,Clark, Kenneth L.,Fechner, Lise,Gore, Paul M.,Hancock, Ashley P.,Hodgson, Simon T.,Holmes, Duncan S.,Kranz, Michael,Looker, Brian E.,Morriss, Karen M. L.,Parton, Daniel L.,Russell, Linda J.,Slack, Robert J.,Sollis, Steven L.,Vile, Sadie,Watts, Clarissa J.
supporting information; experimental part, p. 2183 - 2195 (2011/06/10)
A series of potent phthalazinone-based human H1 and H 3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential treatment of allergic rhinitis, were identified. Blockade of H3 receptors is thought to improve efficacy on nasal congestion, a symptom of allergic rhinitis that is currently not treated by current antihistamines. Two analogues (56a and 56b) had slightly lower H1 potency (pA2 9.1 and 8.9, respectively, vs 9.7 for the clinical gold-standard azelastine, and H3 potency (pK i 9.6 and 9.5, respectively, vs 6.8 for azelastine). Compound 56a had longer duration of action than azelastine, low brain penetration, and low oral bioavailability, which coupled with the predicted low clinical dose, should limit the potential of engaging CNS-related side-effects associated with H 1 or H3 antagonism.
INHIBITORS OF HSP90
-
Page/Page column 62, (2010/04/30)
The invention provides a compound which is (a) a pyrrolopyrimidine derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: Formula (I) wherein R1, R2, R3/
PHENYLPYRAZOLE DERIVATIVES
-
Page/Page column 23-24, (2010/09/05)
The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea sy
NOVEL PIPERIDINE DERIVATIVE
-
Page/Page column 115, (2008/06/13)
Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmac
SUBSTITUTED PYRIDONE DERIVATIVE
-
, (2008/06/13)
Compounds of a formula (I) [wherein, A represents formula (III-1) R3 is a hydrogen, lower alkyl et al; m is 0 or 1; R1 is a hydrogen atom, halogen atom et al, R2 is a hydrogen et al; p is 0 to 4; X is a carbon atom or nitrogen atom; and X1 to X4 is a lowe
COMPOUNDS COMPRISING A LACTAM OR A LACTAM DERIVATIVE MOIETY, PROCESSES FOR MAKING THEM, AND THEIR USES
-
Page/Page column 66, (2008/06/13)
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
CHEMICAL COMPOUNDS
-
Page/Page column 15, (2008/06/13)
Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses (Ia), wherein R1 and R2 are the same or different and represent hydrogen, halogen, -L-O-R3, -L-O-L-A or -L-O-L′-A′, wherein each L is the same or different and represents a direct bond or a C1-C4 alkylene group; L′ represents a direct bond or a C2-C4 alkylene group; R3 represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl; A represents a 5- to 10-membered heterocyclyl group; and A′ represents a C6-C1 aryl group; wherein at least one of R1 and R2 is -L-O-R3, -L-O-L-A or -L-O-L′-A′.
